Journal: Pharmaceutics

Article Title: High-Throughput/High Content Imaging Screen Identifies Novel Small Molecule Inhibitors and Immunoproteasomes as Therapeutic Targets for Chordoma

doi: 10.3390/pharmaceutics15041274

Figure Lengend Snippet: List of cherry-picked compounds. The top 50 compounds were selected as positive hits after the primary screen. Average Z-score and standard deviation between the two replicate plates were considered as criteria for selecting these potential hits. The table shows compounds with different mechanisms of action were qualified for cherry-picking, including the proteasomal inhibitors.

Article Snippet: BNC105 , HY-16114 , −6.33 , 0.346 , BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. , Medchem Express.

Techniques: Standard Deviation, Activity Assay, Expressing, Inhibition, Activation Assay, Histone Deacetylase Assay, Blocking Assay, Binding Assay, Modification, In Vitro

Journal: Pharmaceutics

Article Title: High-Throughput/High Content Imaging Screen Identifies Novel Small Molecule Inhibitors and Immunoproteasomes as Therapeutic Targets for Chordoma

doi: 10.3390/pharmaceutics15041274

Figure Lengend Snippet: Reconfirmation of potential hits from primary assays and dose dependency studies identifies proteasomal inhibitors . ( A – J ) Dose-response curves for cherry-picked compounds from primary screening done in duplicate. ( F ) Dose dependency curves for three proteasomal inhibitors showing reconfirmation of these three inhibitors. ( G , H ) Dose dependency curves for BNC105 and bortezomib or Palbociclib alone or in combination showing low-dose synergistic cell-killing activity of chordoma cells.

Article Snippet: BNC105 , HY-16114 , −6.33 , 0.346 , BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. , Medchem Express.

Techniques: Activity Assay

Journal: Pharmaceutics

Article Title: High-Throughput/High Content Imaging Screen Identifies Novel Small Molecule Inhibitors and Immunoproteasomes as Therapeutic Targets for Chordoma

doi: 10.3390/pharmaceutics15041274

Figure Lengend Snippet: List of IC 50 values for top 10 hits.

Article Snippet: BNC105 , HY-16114 , −6.33 , 0.346 , BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. , Medchem Express.

Techniques:

Journal: Pharmaceutics

Article Title: High-Throughput/High Content Imaging Screen Identifies Novel Small Molecule Inhibitors and Immunoproteasomes as Therapeutic Targets for Chordoma

doi: 10.3390/pharmaceutics15041274

Figure Lengend Snippet: Primary assays identify proteasomal inhibitors as a specific therapeutic agent, alone or in combination with other anti-cancer drugs . ( A – C ) Nuclear count. ( A ) Dose dependency curves for three proteasomal inhibitors showing reconfirmation of these three inhibitors. ( B ) High-dose and ( C ) Low-dose dependency curves for Bortezomib and BNC105 or Palbociclib alone or in combination, showing low-dose synergistic cell-killing activity of chordoma cells. Dose dependency study using proliferation assays ( D ) HEK-293 cells, ( E ) U-CH1 and ( F ) U-CH2 cells alone or ( G ) in combination. ( H ) Percentage cell survival evaluated for BTZ, CFZ, and PKS21265 and the IC 50 values for β5i- and β5c-selective and co-inhibition in U-CH1 cells.

Article Snippet: BNC105 , HY-16114 , −6.33 , 0.346 , BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. , Medchem Express.

Techniques: Activity Assay, Inhibition

Journal: Pharmaceutics

Article Title: High-Throughput/High Content Imaging Screen Identifies Novel Small Molecule Inhibitors and Immunoproteasomes as Therapeutic Targets for Chordoma

doi: 10.3390/pharmaceutics15041274

Figure Lengend Snippet: List of IC 50 values for Bortezomib and anti-cancer drugs in HEK-293 and chordoma cells, individually or in combination.

Article Snippet: BNC105 , HY-16114 , −6.33 , 0.346 , BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. , Medchem Express.

Techniques: